maraviroc Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antivirals CCR5 (Chemokine CC motif receptor 5) receptor antagonists | 1635 | 376348-65-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 8 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 33.37 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 23 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 2.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.25 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 12.80 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 6, 2007 | FDA | VIIV HLTHCARE |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Exposure during pregnancy | 67.05 | 41.21 | 33 | 705 | 108179 | 46577145 |
| Abortion spontaneous | 65.85 | 41.21 | 25 | 713 | 43621 | 46641703 |
| Pathogen resistance | 61.05 | 41.21 | 15 | 723 | 6045 | 46679279 |
| CSF test abnormal | 50.38 | 41.21 | 8 | 730 | 337 | 46684987 |
| Generalised anxiety disorder | 49.52 | 41.21 | 10 | 728 | 1650 | 46683674 |
| Live birth | 48.61 | 41.21 | 14 | 724 | 10316 | 46675008 |
| Viral mutation identified | 48.18 | 41.21 | 10 | 728 | 1889 | 46683435 |
| Social avoidant behaviour | 44.18 | 41.21 | 10 | 728 | 2829 | 46682495 |
| Hyperbilirubinaemia | 44.05 | 41.21 | 13 | 725 | 10425 | 46674899 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Virologic failure | 141.97 | 23.80 | 35 | 2070 | 3184 | 29947189 |
| Viral mutation identified | 107.97 | 23.80 | 27 | 2078 | 2599 | 29947774 |
| Immune reconstitution inflammatory syndrome | 63.77 | 23.80 | 24 | 2081 | 9077 | 29941296 |
| Progressive multifocal leukoencephalopathy | 46.33 | 23.80 | 19 | 2086 | 8994 | 29941379 |
| Drug resistance | 45.48 | 23.80 | 24 | 2081 | 20109 | 29930264 |
| Pathogen resistance | 44.16 | 23.80 | 18 | 2087 | 8392 | 29941981 |
| Viral load increased | 41.47 | 23.80 | 13 | 2092 | 2841 | 29947532 |
| Lipodystrophy acquired | 38.65 | 23.80 | 13 | 2092 | 3547 | 29946826 |
| Enanthema | 37.19 | 23.80 | 8 | 2097 | 395 | 29949978 |
| CSF HIV escape syndrome | 33.37 | 23.80 | 6 | 2099 | 115 | 29950258 |
| Blood HIV RNULL increased | 31.66 | 23.80 | 9 | 2096 | 1407 | 29948966 |
| Anal cancer | 31.00 | 23.80 | 7 | 2098 | 433 | 29949940 |
| Hodgkin's disease | 30.52 | 23.80 | 8 | 2097 | 924 | 29949449 |
| Drug interaction | 30.51 | 23.80 | 52 | 2053 | 199516 | 29750857 |
| Congenital renal disorder | 29.09 | 23.80 | 5 | 2100 | 73 | 29950300 |
| Congenital ureteric anomaly | 27.82 | 23.80 | 4 | 2101 | 16 | 29950357 |
| Kidney enlargement | 27.01 | 23.80 | 7 | 2098 | 773 | 29949600 |
| Congenital vesicoureteric reflux | 25.94 | 23.80 | 4 | 2101 | 28 | 29950345 |
| Acquired immunodeficiency syndrome | 24.72 | 23.80 | 6 | 2099 | 508 | 29949865 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AX09 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals |
| FDA MoA | N0000175445 | Chemokine Co-receptor 5 Antagonists |
| FDA EPC | N0000175572 | CCR5 Co-receptor Antagonist |
| MeSH PA | D019380 | Anti-HIV Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D044966 | Anti-Retroviral Agents |
| MeSH PA | D000998 | Antiviral Agents |
| MeSH PA | D065100 | CCR5 Receptor Antagonists |
| MeSH PA | D023581 | HIV Fusion Inhibitors |
| CHEBI has role | CHEBI:36044 | anti-virus drug |
| CHEBI has role | CHEBI:59886 | hiv entry inhibitors |
| CHEBI has role | CHEBI:63673 | chemokine receptor 5 antagonists |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| CCR5 Tropic Drug Resistant HIV Infection | indication | ||
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Orthostatic hypotension | contraindication | 28651003 | |
| Infectious disease | contraindication | 40733004 | |
| Viral hepatitis C | contraindication | 50711007 | DOID:1883 |
| Acute nephropathy | contraindication | 58574008 | |
| Chronic type B viral hepatitis | contraindication | 61977001 | |
| Chronic renal failure syndrome | contraindication | 90688005 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Drug-induced hepatitis | contraindication | 235876009 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Myocardial ischemia | contraindication | 414795007 | DOID:3393 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.8 | Basic |
| pKa2 | 5.07 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 20MG/ML | SELZENTRY | VIIV HLTHCARE | N208984 | Nov. 4, 2016 | RX | SOLUTION | ORAL | Oct. 30, 2023 | NEW PATIENT POPULATION |
| 20MG/ML | SELZENTRY | VIIV HLTHCARE | N208984 | Nov. 4, 2016 | RX | SOLUTION | ORAL | April 30, 2024 | PEDIATRIC EXCLUSIVITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| C-C chemokine receptor type 5 | GPCR | ANTAGONIST | Kd | 7.60 | CHEMBL | CHEMBL | |||
| Multidrug and toxin extrusion protein 1 | Transporter | IC50 | 4.76 | CHEMBL | |||||
| C-C chemokine receptor type 5 | GPCR | Ki | 9.62 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4026629 | VUID |
| N0000179791 | NUI |
| D06670 | KEGG_DRUG |
| 4026629 | VANDF |
| C1964465 | UMLSCUI |
| CHEBI:63608 | CHEBI |
| CHEMBL1201187 | ChEMBL_ID |
| D000077592 | MESH_DESCRIPTOR_UI |
| DB04835 | DRUGBANK_ID |
| 3002977 | PUBCHEM_CID |
| 806 | IUPHAR_LIGAND_ID |
| 8450 | INN_ID |
| MD6P741W8A | UNII |
| 620216 | RXNORM |
| 118030 | MMSL |
| 24072 | MMSL |
| d06852 | MMSL |
| 012282 | NDDF |
| 427805000 | SNOMEDCT_US |
| 429603001 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-223 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 31 sections |
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-224 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 31 sections |
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-233 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 31 sections |
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-235 | TABLET, FILM COATED | 75 mg | ORAL | NDA | 31 sections |
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49702-237 | SOLUTION | 20 mg | ORAL | NDA | 31 sections |
| SELZENTRY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5809 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 32 sections |